(57) A compound having the formula
wherein
R is hydrogen, (C₁-C₃)alkyl, phenyl, benzyl or a conventional radical forming an ester
group which is hydrolyzable under physiological conditions;
X is F, Cl, Br, I, (C₁-C₃)alkyl, CF₃, benzyl, (C₁-C₃)alkoxy, (C₂-C₄)alkanoyloxy or
(C₂-C₄)alkoxycarbonyl; and
X¹, X² and X³ are each independently hydrogen, F, Cl, Br, I, (C₁-C₃)alkyl, CF₃, benzyl,
(C₁-C₃)alkoxy, (C₂-C₄)alkanoyloxy or (C₂-C₄)alkoxycarbonyl; or
a pharmaceutically acceptable cationic salt thereof when R is hydrogen.
2. A compound of claim 1 wherein R is a radical selected from the group consisting
of:
furan-5(1H)-on-1-yl;
isobenzofuran-3(1H)-on-1-yl;
3,4-dihydrofuran-5(1H)-on-1-yl;
-CHR¹OCOR², and
-CHR¹OCOOR²;
wherein
R¹ is hydrogen or methyl; and
R² is (C₁-C₆)alkyl.
3. A compound of claim 1 wherein R is hydrogen, (C₁-C₃)alkyl, phenyl or benzyl.
4. A compound of claim 3 wherein R is hydrogen.
5. The compound of claim 4 wherein X is 3-methyl, X¹ is 5-methyl, X³ is 3′-methyl
and X⁴ is 4′-fluoro.
The compounds are blood cholesterol lowering agents and so are useful in the prevention
and treatment or cardiovascular diseases such as atherosclerosis.
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